Bromodomain and extraterminal protein inhibitors in pediatrics: A review of the literature

Pediatr Blood Cancer. 2017 May;64(5). doi: 10.1002/pbc.26334. Epub 2016 Nov 30.

Abstract

The last few years have seen the identification of pharmacologic approaches to target bromodomain and extraterminal (BET) proteins for cancer treatment. These proteins have an essential role in gene transcription regulation by binding acetylated lysine residues on histone tails, activating gene transcription. BET inhibitors have been tested in preclinical models including pediatric malignancies and several adult clinical trials are ongoing. Since the development of new drugs in pediatric cancer has long lagged behind programs for adults, the aim of this review is to show the importance of these therapies in pediatric malignancies to support their development in pediatric oncology/hematology.

Keywords: BET inhibitors; bromodomain; epigenetics; pediatrics.

Publication types

  • Review

MeSH terms

  • Antineoplastic Agents / therapeutic use
  • Brain Neoplasms / drug therapy*
  • Cell Cycle Proteins
  • Child
  • Child, Preschool
  • Hematologic Neoplasms / drug therapy*
  • Humans
  • Neuroblastoma / drug therapy*
  • Nuclear Proteins / antagonists & inhibitors*
  • Protein Serine-Threonine Kinases / antagonists & inhibitors*
  • RNA-Binding Proteins / antagonists & inhibitors*
  • Transcription Factors / antagonists & inhibitors*
  • Transcriptional Activation / drug effects

Substances

  • Antineoplastic Agents
  • BRD2 protein, human
  • BRD3 protein, human
  • BRD4 protein, human
  • BRDT protein, human
  • Cell Cycle Proteins
  • Nuclear Proteins
  • RNA-Binding Proteins
  • Transcription Factors
  • Protein Serine-Threonine Kinases